Is it possible there are still many more receptors and agonists to discover inside the human body

I’m not sure if this is a gq, I assume so.

With 2016 medical technology is it possible there are still endless receptors within the human body as well as agonists, antagonists, inverse agonists etc that we haven’t discovered yet, or have we mostly figured them out?

I’ve heard that even though there are only about 25k genes in the human body, there could be over a million different proteins. Not only that but a lot of receptor agonists (adrenaline, neurotransmitters, etc) are not proteins.

So are scientists still discovering new receptors and their agonists inside the human body, or have they mostly all been found?

Who knows what will or won’t be discovered but personally I’d be surprised if there were not more identified and currently thought of as single ones redefined into various subgroups.

For example the hormone leptin was just discovered in 1994 and its receptor in 1995. Delineating subtypes of those receptors and how they each work is a work still in progress. Quick googling finds new receptors that have been discovered in 2014 and in 2016. Heck even new whole classes of receptors as recently as 2014.

No GQ answer that can promise that that’s not it, but it would be pretty shocking.

The more we know about the human body and cell physiology, the less we realize we really do know.

The answer is yes.

A very wide variety of living creatures can sense magnetic fields and use the sense to navigate. Some scientists think that humans also have magnetoreception. This might not even require a new protein: human retina already has the cryptochrome(s) with the special quantum properties key to magnetoreception.

Considering that it was only just demonstrated that we have a lymphatic system in the brain, yes.

Depends on what you are looking at - since we know the sequence of the human genome, we know how many potential genes there are, e.g. of G-protein coupled receptors or Tyrosine-kinase containing receptors. However, some cell surface proteins do not have endogenous signalling capacity, but interact non-covalently with other proteins upon activation, so they can only be recognized as signaling receptors by biochemical characterization.

The genome does not tell us what ligands are recognized by these receptors. Amongst the potential ligands, there are proteins, small peptidic fragments of proteins, and a large number of non-peptidic ligands. Besides the endogenous ligands produced by our body, many non-endogenous substances are of medical interest. Often, the ligands used by our body do not make very good drugs, and many of the agonists, antagonists and inverse agonists to pharmacologically relevant receptors are compounds produced in the laboratory, isolated from plants or produced by microorganisms.

So: There are not endless receptors in our body, the receptors are a subset of all proteins in our body. If you include artificial ligands, the number of possible ligands is not so limited. Substances capable of interacting with a particular receptor need to have a substructure complementary to the binding pocket of the receptor, but other parts of the molecule can be widely varied.

But there are many chemicals in our bodies which aren’t proteins, too. Some are modified proteins (like the iron-containing hemoglobin), and some are completely different sorts of chemical (ATP, lipids, nucleic acids, polysaccharides, etc.). Couldn’t receptors be one of those non-protein chemicals, too?

This is NOT my area of expertise.

I read (and sometimes even comprehend) this blog by a medicinal chemist: http://blogs.sciencemag.org/pipeline/

My interpretation of his, and his commenters, writings over the last few years is that we’ve barely scratched the surface on all the signaling pathways in human biology.

Some types of signaling systems are decently understood. Other areas haven’t even been found yet, much less explored or tamed.

I can claim some expertise on some of the well-known cell signalling pathways, but nobody can be an expert on the unknown pathways…

My WAG is that there are still plenty of undiscovered pathways. Last year I was at a conference where someone gave a talk where, incidental to their main project looking for tumor suppressors in a fruit fly model, they discovered the receptor for a protein known to be involved in axon guidance in humans.

When the OP mentions “millions of different proteins”, they’re typically talking about alternative splicing (cutting and pasting messenger RNA in different ways to make different proteins) and post-translational modifications of proteins. I can assure you that there’s still plenty to learn about the gory details of post-translational modifications. My thesis project* is about how a particular class of post-translational modifications regulates the activity one specific signaling protein. Every few days I read a new paper about intricate details about how specific post-translational modifications are involved in the regulation of my pathway of interest. E.g., modification A of signaling protein X disables it, but modification B blocks modification A.

*holy crap why am I here and not writing?!?

My understanding is that when it comes to biology on the macro scale, there really isn’t much more to learn. Meaning, pretty much all the macro structures have been identified. New muscles, tendons, ligaments, major nerves and arteries, etc. are not being constantly discovered.

However, does cellular biology drastically lag behind macrobiology (or whatever it is called)? I thought cellular biology was a very advanced field. Maybe not.

I’d even start with questioning your first premise.

The interactions between multiple large systems within the body are still being defined - just think about the major work being done with the very large system that is the microbiome and how it interacts with the immune system, the gut, even the brain. The idea that the microbiome has so much to do with regulating those (and being regulated by those) other “macro” systems is grand scale very recent.

Of course the details of how it does so is parsed out in hundreds of thousands of details at the level of cellular biology.

Even at the level of human anatomy there are still areas of active research and new discovery. The role of fasciae, for instance, on joint flexibility, muscle stiffness and pain, proprioception, and immune system response, is an area of active research today, whereas a decade ago it was largely considered to be just inner dermis and interstitial tissue that was largely inert. Similarly, connections between the centeral, autonomic, lymphatic, and enteric nervous system are still being discovered which give better understanding of how diet affects other organ function, immune response, and cognitive function beyond just providing energy (carbohydrates) and structural materials (proteins and lipids). There are many details of retinal function that are still in research, and a few years ago a purported new layer of the cornea (“Dua’s lawyer”) was presented in a paper, although there is still dispute about whether it should be considered a separate part. Someone already mentioned the previously unsuspected lymphatic network in the meningeneal linkings of the cranium. And all of that is in the most extensively researched large mammal; there is plenty of anatomical and physiological features and mechanisms in other animals that are poorly understood.

Molecular biology is a diverse field of enormous complexity and we are only now starting to develop refined enough models and sophisticated computational tools and methods to begin to simulate entire cells, and even at that many processes are represented as empirical ‘black boxes’ due to limitations in simulation of protein conformation and how the similar proteins can have completely different effects on various receptors or other proteins (protein-to-protein interactions) which govern cellular metabolism, cell development and differentiation, and various intercellular processes which regulate anabolism and catabolism (internal assembly and disassembly) of parts of the cell. Cell biology–the summa totalis of cellular function, analagous to anatomy and physiology at the macroscopic organism level–is a superset of molecular biology but also includes complex interactions with the ‘outside world’ (e.g. the organism they make up, and even the environment beyond) which leads to so-called ‘systems biology’, which is such an overwhelmingly complex field that it can barely be called a real science at this point. Much of the hypotheses of systems biology are, like cosmology, really beyond controlled experiment or observation.

The human (or other complex animal) physiology is such a phenomenally complicated system that it is difficult to imagine a point at which there will be nothing left to study or discover. Until we get to the point that we could literally synthesize up a human body from raw materials (chemical elements, mineral compounds, and amino acits) and make it function in every way that a human being does, we can scarcely be said to be done with biology as an area of research. And we are far, far away from even being able to completely synthesize even very simple organisms. The best we’ve done to date in synthetic biology are synthesized genomes (albeit based upon largely existing genomic structures) and self-assembling proteins which, while fascinating, nobody considers to be living organisms.

Stranger

Not necessarily. Recall:

Bolding mine: Alternative splicing - Wikipedia

One gene can lead to many very different polypeptides with different functions. And these polypeptides may each go on to be folded differently or functionalized differently.

What I don’t have, however, is an example of different receptors from one gene that interact with different agonists.

And not all molecules with protein-like function are primarily composed of amino acids, see ribozymes.

Somewhat tangentially but very cool is the potentially completely additional set of ways in which information may be encoded by way of control of certain folding processes by of endogenous prions. This one example, CPEB3, is, one suspects, just the first one found.

The amount that is unknown but potentially knowable is vast and the more that becomes known the more aware the scientific community becomes of how much more there is to know.

I believe it’s only been in the last decade or so that scientists have discovered taste receptors all over the human body, including the lungs, digestive system, pancreas, and testes. Their functions are only partially understood.

One issue I’m unsure of is the history of the clitoris. Depending on where you look, the clitoris was either fully described by Georg Kobelt in the 1840s or Helen O’Connell in the late 1990s. I think O’Connell was studying the nerves to the clitoris, but she got tied up in the politics of how the clitoris is described in anatomy textbooks, that is, it’s much more than the glans and extends deep into the body, but she didn’t discover that, did she? Did she discover new nerves? Or what?

Throughout the 2000s there were all sorts of studies trying to prove or disprove the existence of the G-spot. AFAIK the current framework is there’s a so called CUV (clitourethrovaginal) complex. That this sort of stuff is only being discovered recently is…interesting.

Terms: Receptors are proteins folded in a certain way with sometimes added parts to make the “pocket”.
Agonists and antagonists are natural or unnatural molecules that go into the pocket. There is no limit to molecules we can make. See for example

And the receptors it works at.

I’ve been mulling over the topic these last few days and have some more comments (On the off chance that anyone is still interested…) One major point to keep in mind is that biology is the study of insanely complex systems which are not the result of a rational designer. In such systems, very subtle details can be absolutely critical for understanding how the system functions.

It is advanced in some ways. We’ve learned an awful lot over the last several decades, and can tell all sorts of stories about how cells behave. But our understanding is largely qualitative. That’s led to the enumeration of (probably) most of cell signaling pathways, and a general understanding of how those pathways work. For instance, in developmental biology, using model organism genetics we’ve been able to enumerate nearly every mutation that screws up embryonic development. That work led to the discovery of many conserved signaling pathways, and subsequent work has worked out the general outlines of each pathway, which are usually the same in all animals. To answer the question in the OP directly, I’d say these approaches have probably identified a large majority of the signals and receptors in the human genome.

However, our quantitative understanding of most pathways is very poor. When I started research I was very enthusiastic about mathematical models of cell signaling pathways. Now that I’m familiar with the gory biochemical details, I’m less impressed. The models that exist rely on a lot of approximations and empirical fudging, because we can’t measure relevant biochemical parameters in sufficient detail.

For instance, if you knew concentrations, catalysis rates, and dissociation constants for every set of interacting proteins in a pathway, you ought to be able to make a pretty good model of how signals are transmitted through the pathway. But we can’t measure those in a cell. Most of our biochemical techniques require huge amounts of purified proteins to measure those parameters in isolated, artificial conditions. Even worse, those measurements aren’t even very consistent – I’ve seen measurements of receptor-ligand binding that differ by orders of magnitude. And that was with a system were ligand dimers interact with receptor tetramers. If we can’t reliably measure the interaction between one ligand and one receptor, how the hell can we predict the relative interaction between a dimer composed of two different ligands and four different receptors? When there are also half dozen or so co-receptors and antagonists, all interacting at the same time and place?

And those are the best techniques. Most of the techniques I’m using right now come down to “is this blob darker or smaller than that blob?”

There’s a famous essay on the inadequacy of biological approaches to fully understand the systems we study: “Can A Biologist Fix A Radio?” That essay makes some very good points about how we can only learn so much about a system when our most of our best approaches ultimately come down to breaking it and describing the results. However, while I can agree with the desire for a better quantitative understanding, we simply lack the tools to do so with sufficient accuracy. To take the radio analogy further, let’s say that we can figure out how all the components are wired. But we can’t measure the basic properties of most of the components, and the few measurements that are possible are wildly inaccurate. What the hell use is a circuit diagram where we can measure most of the capacitors with decent accuracy, half of the resistors within two orders of magnitude, and none of the inductors, and don’t even know about the existence of diodes?

It’s very common for the cell signaling pathways I’m familiar with, which actually include large “families” of ligands and receptors. In many cases, one receptor can be activated by multiple ligands. For example, the EGF receptor (EGFR) can be activated by both EGF and TGF-α (as well as a host of other EGF family ligands).

To get back to the OP, EGFR activation is a good example of how subtle differences in protein interactions can lead to very different system behaviors. EGFR is a receptor tyrosine kinase. Conceptually, it has one of the simplest methods of receptor activation: in absence of EGF, the receptors don’t interact. When EGF is present, the extracellular domains of EGFR stick to each other, bringing the intracellular kinase domains close enough to interact, which allows them to phosphorylate each other and downstream signaling proteins.

Naively, you might then think that any way to get two EGFR proteins close enough to activate each other would be equivalent. But that’s not the case. In certain cell types, TGF-α can cause cancerous proliferation, but EGF does not. Yet, both bind to EGFR with similar dissociation constants, and result in similar levels of receptor phosphorylation. How can this be? I’ve read some very fascinating structural biology papers showing how EGF and TGF-α binding cause very subtlly different changes in the structure of the EGFR intracellular domain. It seems to be a matter of two short helices, outside the EGFR catalytic domain, that adopt slightly different orientations when bound by EGF and TGF-α. That in turn, results in a very different output: EGF-bound EGFR is taken into the cell and degraded, but TGF-α-bound EGFR stays on the cell surface and remains active.

That’s the sort of subtle detail that, in human terms, means the difference between cancer and normal wound healing. And since protein structure prediction is still not a solved problem, it’s not yet possible to predict such differences even in the case of one receptor that binds two ligands.

And this is just a single pathway. There are all sorts of ways for different pathways to interact with each other, at multiple levels.

That wall of text deserves a tl;dr: Biology is complicated. We’ve probably identified most cell signaling ligands, agonists, and receptors, but we can only describe their behavior in qualitative terms.

Is this an example of two receptors from one gene?

Nope. Sorry, didn’t parse your statement correctly. Two ligands produced by separate genes, one receptor, no alternative splicing of consequence.

Alternative splicing isn’t quite as wide-spread in the model organisms I’m familiar with… and from all the examples I can think of off the top of my head, it’s the intracellular domain that differs.

I recalled that integrins are a receptor of sorts, with gigantic extracellular domains that have multiple splice variants, and relatively small and simple intracellular domains. After a bit of searching, I found a few examples where different receptor splice variants have different extracellular ligands.

In one case, integrin α7 splice variant x1 binds to laminin 1 and 2, while the splice variant x2 binds to laminin 2, 8, 10, and 11. (Reference - note that the laminin “isoforms” the paper refers to are not splice variants, and instead refer to different combinations of polypeptide subunits which are not produced by alternative splicing in this exact case.)

There are a ton of other examples of tissue-specific expression of particular integrin splice variants, which sometimes produce integrins with different extracellular protein binding domains.